Synthesis of metabolically blocked paclitaxel analogues

M D Wittman; T J Altstadt; C Fairchild; S Hansel; K Johnston; J F Kadow; B H Long; W C Rose; D M Vyas; M J Wu; M E Zoeckler

doi:10.1016/s0960-894x(01)00066-x

Synthesis of metabolically blocked paclitaxel analogues

Bioorg Med Chem Lett. 2001 Mar 26;11(6):809-10. doi: 10.1016/s0960-894x(01)00066-x.

Authors

M D Wittman¹, T J Altstadt, C Fairchild, S Hansel, K Johnston, J F Kadow, B H Long, W C Rose, D M Vyas, M J Wu, M E Zoeckler

Affiliation

¹ Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492-7660, USA. [email protected]

PMID: 11277525
DOI: 10.1016/s0960-894x(01)00066-x

Abstract

The stereospecific syntheses of the metabolically blocked 6-alpha-F, Cl, Br paclitaxel, and 6-alpha-F-10-acetyldocetaxel are described and in vitro and in vivo activity is presented.

MeSH terms

Antineoplastic Agents, Phytogenic / chemical synthesis
Antineoplastic Agents, Phytogenic / chemistry
Antineoplastic Agents, Phytogenic / metabolism
Antineoplastic Agents, Phytogenic / pharmacology
Drug Stability
Humans
Inhibitory Concentration 50
Paclitaxel / analogs & derivatives
Paclitaxel / chemical synthesis*
Paclitaxel / chemistry
Paclitaxel / metabolism
Paclitaxel / pharmacology
Taxoids*
Tumor Cells, Cultured

Substances

6-fluoro-10-acetyldocetaxel
Antineoplastic Agents, Phytogenic
Taxoids
Paclitaxel